Evidence map›Paper›PMID 33370295›Full record

ArticlePloS one2020

Antileishmanial activity of synthetic analogs of the naturally occurring quinolone alkaloid N-methyl-8-methoxyflindersin.

Elaine Torres Suarez, Diana Susana Granados-Falla, Sara María Robledo, Javier Murillo, Yulieth Upegui, Gabriela Delgado

Open access · goldAbstract read
In one paragraph

Article in PloS one, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
2.0field-weighted citation impact, top 12% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

9 citing papers in PubMed, 15 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Review
  5. Article
  6. Article
  7. Review
  8. High Selectivity of 8-Hydroxyquinoline onPharmaceuticals (Basel, Switzerland) · 2023
    Article
  9. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors at 3 institutions in 1 country.

Elaine Torres SuarezGrupo de Investigación en Inmunotoxicología, Departamento de Farmacia, Universidad Nacional de Colombia, Bogotá, Colombia.
Diana Susana Granados-FallaGrupo de Investigación en Inmunotoxicología, Departamento de Farmacia, Universidad Nacional de Colombia, Bogotá, Colombia.
Sara María RobledoPECET, Facultad de Medicina, Universidad de Antioquia, Medellín, Colombia.
Javier MurilloPECET, Facultad de Medicina, Universidad de Antioquia, Medellín, Colombia.
Yulieth UpeguiPECET, Facultad de Medicina, Universidad de Antioquia, Medellín, Colombia.
Gabriela DelgadoGrupo de Investigación en Inmunotoxicología, Departamento de Farmacia, Universidad Nacional de Colombia, Bogotá, Colombia.ORCID 0000-0003-2947-7796
Universidad de Antioquia · COUniversidad Nacional de Colombia · COUniversidad El Bosque · CO

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Leishmaniasis is a neglected, parasitic tropical disease caused by an intracellular protozoan from the genus Leishmania. Quinoline alkaloids, secondary metabolites found in plants from the Rutaceae family, have antiparasitic activity against Leishmania sp. N-methyl-8-methoxyflindersin (1), isolated from the leaves of Raputia heptaphylla and also known as 7-methoxy-2,2-dimethyl-2H,5H,6H-pyran[3,2-c]quinolin-5-one, shows antiparasitic activity against Leishmania promastigotes and amastigotes. This study used in silico tools to identify synthetic quinoline alkaloids having structure similar to that of compound 1 and then tested these quinoline alkaloids for their in vitro antiparasitic activity against Leishmania (Viannia) panamensis, in vivo therapeutic response in hamsters suffering from experimental cutaneous leishmaniasis (CL), and ex vivo immunomodulatory potential in healthy donors' human peripheral blood (monocyte)-derived macrophages (hMDMs). Compounds 1 (natural), 2 (synthetic), and 8 (synthetic) were effective against intracellular promastigotes (9.9, 3.4, and 1.6 μg/mL medial effective concentration [EC50], respectively) and amastigotes (5.07, 7.94, and 1.91 μg/mL EC50, respectively). Compound 1 increased nitric oxide production in infected hMDMs and triggered necrosis-related ultrastructural alterations in intracellular amastigotes, while compound 2 stimulated oxidative breakdown in hMDMs and caused ultrastructural alterations in the parasite 4 h posttreatment, and compound 8 failed to induce macrophage modulation but selectively induced apoptosis of infected hMDMs and alterations in the intracellular parasite ultrastructure. In addition, synthetic compounds 2 and 8 improved the health of hamsters suffering from experimental CL, without evidence of treatment-associated adverse toxic effects. Therefore, synthetic compounds 2 and 8 are potential therapeutic candidates for topical treatment of CL.

Indexed as

AlkaloidsAnimalsAntiprotozoal AgentsCricetinaeDisease Models, AnimalHeterocyclic Compounds, 3-RingHumansLeishmania guyanensisLeishmaniasis, CutaneousMacrophagesMiceNitric OxidePlant LeavesQuinolinesQuinolonesRutaceaeAlkaloidsAntiprotozoal AgentsflindersineHeterocyclic Compounds, 3-RingNitric OxidequinolineQuinolinesQuinolones

Identifiers

PMID33370295
PMCPMC7769561
OpenAlexW3115247077

What OpenQuestion holds

Textmetadata
LicenceCC BY
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.